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Elimusertib hydrochloride
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Elimusertib hydrochloride图片
包装与价格：
包装 价格(元)
10 mM * 1 mL in DMSO 电议
2mg 电议
5mg 电议
10mg 电议
25mg 电议
50mg 电议
100mg 电议
200mg 电议
500mg 电议

半岛bd体育手机客户端 名称
BAY 1895344 hydrochloride
半岛bd体育手机客户端 介绍
Elimusertib (BAY 1895344) hydrochloride 是一种有效、可口服、选择性的 ATR抑制剂， IC50值为 7 nM，具有抗肿瘤活性。Elimusertib hydrochloride 可用于实体瘤和淋巴瘤的研究。
生物活性

Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selectiveATRinhibitor with anIC50of 7 nM. Elimusertib hydrochloride has anti-tumor activity[1][2]. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas[3].
IC50& Target[1]

ATR

7 nM (IC50)
体外研究
(In Vitro)

Elimusertib hydrochloride potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC50of 78 nM[1].
Elimusertib hydrochloride potently suppresses hydroxyurea-induced H2AX phosphorylation (IC50: 36 nM)[1].
Elimusertib hydrochloride shows good selectivity against mTOR (ratio of IC50values: mTOR/ATR 61)[3].
Elimusertib hydrochloride reveals high selectivity against other related kinases, such as DNA-PK (IC50: 332 nM), ATM (IC50: 1420 nM), and PI3K (IC50: 3270 nM)[3].
Elimusertib hydrochloride has potent antiproliferative activity against various cancer cell lines in vitro, 25 for example in the CRC cell lines HT-29 (IC50: 160 nM) and LoVo (IC50: 71 nM), and in the B-cell lymphoma cell line SU-DHL-8 (IC50: 9 nM)[3].
体内研究
(In Vivo)

Elimusertib hydrochloride shows potent anti-tumor efficacy in monotherapy in a variety of xenograft models of ovarian and colorectal cancer, and causes complete tumor remission in mantle cell lymphoma models[2].
Elimusertib hydrochloride (50 mg/kg; p.o.; b.i.d.; 3 days on/4 days off; for 11 days) exhibits strong antitumor efficacy in the ATM-mutated SU-DHL-8 (ATM K1964E) human GCB-DLBCL cell line derived xenograft model in mice[3].
Elimusertib hydrochloride (20 mg/kg, and 10 mg/kg from day 14; p.o.; daily; 2 days on/5 days off; for 42 days) in combination with Carboplatin (40 mg/kg; i.p.; daily; 1 day on/6 days off) results in synergistic antitumor activity in the platinum-resistant ATM protein low expressing CR5038 human CRC PDX model in NOD/SCID mice[3].
Elimusertib hydrochloride exhibits moderate oral bioavailability (rat 87%, dog 51%) following oral administration (rat and dog 0.6-1 mg/kg)[3].
Elimusertib hydrochloride exhibits terminal elimination half-lives (mouse 0.17 h, rat 1.3 and, dog 1.0 h) due to plasma clearance (3.5, 1.2, and 0.79 L/h/kg respectively) following intravenous administration (mouse, rat and dog 0.3-0.5 mg/kg)[3].

Animal Model: Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model[3]
Dosage: 50 mg/kg
Administration: Oral administration, b.i.d., 3 days on/4 days off, for 11 days
Result: Inhibited tumor area.
Animal Model: Male Wistar rats[3]
Dosage: 0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration
Result: Oral bioavailability (87%), T1/2(1.3 h).
Animal Model: Female beagle dogs[3]
Dosage: 0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration
Result: Oral bioavailability (51%), T1/2(1.0 h).
Clinical Trial
分子量

411.89
性状

Solid
Formula

C20H22ClN7O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:

DMSO : 50 mg/mL(121.39 mM;Need ultrasonic)

H2O : 50 mg/mL(121.39 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.4278 mL 12.1392 mL 24.2783 mL
5 mM 0.4856 mL 2.4278 mL 4.8557 mL
10 mM 0.2428 mL 1.2139 mL 2.4278 mL
*

请根据半岛bd体育手机客户端 在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的半岛bd体育手机客户端 失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： PBS

    Solubility: 100 mg/mL (242.78 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO40%PEG3005%Tween-8045% saline

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.05 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂： 10% DMSO90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.05 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 4.

    请依序添加每种溶剂： 10% DMSO90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

* 以上所有助溶剂都可在本网站选购。
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